Deshayes Stephanie, Xian Wujing, Schmidt Nathan W, Kordbacheh Shadi, Lieng Juelline, Wang Jennifer, Zarmer Sandra, Germain Samantha St, Voyen Laura, Thulin Julia, Wong Gerard C L, Kasko Andrea M
Department of Pharmaceutical Chemistry, University of California, San Francisco , 555 Mission Bay Boulevard South, San Francisco, California 94158, United States.
Bioconjug Chem. 2017 Mar 15;28(3):793-804. doi: 10.1021/acs.bioconjchem.6b00725. Epub 2017 Mar 1.
We design hybrid antibiotic peptide conjugates that can permeate membranes. Integration of multiple components with different functions into a single molecule is often problematic, due to competing chemical requirements for different functions and to mutual interference. By examining the structure of antimicrobial peptides (AMPs), we show that it is possible to design and synthesize membrane active antibiotic peptide conjugates (MAAPCs) that synergistically combine multiple forms of antimicrobial activity, resulting in unusually strong activity against persistent bacterial strains.
我们设计了能够穿透细胞膜的杂合抗生素肽缀合物。由于不同功能对化学条件的竞争以及相互干扰，将多种具有不同功能的组分整合到单个分子中往往存在问题。通过研究抗菌肽（AMPs）的结构，我们表明可以设计并合成膜活性抗生素肽缀合物（MAAPCs），这些缀合物能协同结合多种抗菌活性形式，从而对持续性细菌菌株产生异常强大的活性。
